JP2005505571A5 - - Google Patents

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Publication number
JP2005505571A5
JP2005505571A5 JP2003528769A JP2003528769A JP2005505571A5 JP 2005505571 A5 JP2005505571 A5 JP 2005505571A5 JP 2003528769 A JP2003528769 A JP 2003528769A JP 2003528769 A JP2003528769 A JP 2003528769A JP 2005505571 A5 JP2005505571 A5 JP 2005505571A5
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Japan
Prior art keywords
compound
alkyl
compound according
hydrogen
solvate
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JP2003528769A
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Japanese (ja)
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JP2005505571A (en
JP4421293B2 (en
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Priority claimed from PCT/EP2002/010179 external-priority patent/WO2003024921A1/en
Publication of JP2005505571A publication Critical patent/JP2005505571A/en
Publication of JP2005505571A5 publication Critical patent/JP2005505571A5/ja
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Publication of JP4421293B2 publication Critical patent/JP4421293B2/en
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Expired - Fee Related legal-status Critical Current

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Claims (20)

構造式(I):
Figure 2005505571

(式中、
nは0〜2の整数であり;
Xは、S、O又はNR34であり;
3及びR4は、独立して、水素、アルキル、アリール、アリールアルキル、シクロアルキル若しくはシクロアルキル−アルキルであるか、又はそれらが結合している窒素原子と一緒になってヘテロシクリル環を形成し;
Yは、−OR5、−SR5又は−NR67であり;
5は、水素、アルキル、アリール、アリールアルキル、シクロアルキル又はシクロアルキル−アルキルであり;
6及びR7は、互いに独立して、水素、アルキル、アリール、アリールアルキル、シクロアルキル若しくはシクロアルキル−アルキルであるか、又はそれらが結合している窒素原子と一緒になってヘテロシクリル環を形成し;
1は、(C2〜C8)アルキルであり;
2は、水素、アルキル、ヒドロキシ又はオキソであり;そして
9は、水素、アルキル、ハロアルキル、ハロ、シアノ、ニトロ又はアルコキシである)
で示される化合物、あるいはその塩、溶媒和物又は水和物。
Structural formula (I):
Figure 2005505571

(Where
n is an integer from 0 to 2;
X is S, O or NR 3 R 4 ;
R 3 and R 4 are independently hydrogen, alkyl, aryl, arylalkyl, cycloalkyl or cycloalkyl-alkyl, or together with the nitrogen atom to which they are attached, form a heterocyclyl ring. ;
Y is —OR 5 , —SR 5 or —NR 6 R 7 ;
R 5 is hydrogen, alkyl, aryl, arylalkyl, cycloalkyl or cycloalkyl-alkyl;
R 6 and R 7 , independently of one another, are hydrogen, alkyl, aryl, arylalkyl, cycloalkyl or cycloalkyl-alkyl or together with the nitrogen atom to which they are attached form a heterocyclyl ring And
R 1 is (C 2 -C 8 ) alkyl;
R 2 is hydrogen, alkyl, hydroxy or oxo; and R 9 is hydrogen, alkyl, haloalkyl, halo, cyano, nitro or alkoxy)
Or a salt, solvate or hydrate thereof.
nが1である、請求項1記載の化合物。   The compound according to claim 1, wherein n is 1. 2が水素である、請求項1記載の化合物。 The compound of claim 1, wherein R 2 is hydrogen. XがOである、請求項1記載の化合物。   The compound of claim 1, wherein X is O. YがOHである、請求項1記載の化合物。   The compound of claim 1, wherein Y is OH. 1が(C4〜C8)アルキルである、請求項1記載の化合物。 The compound of claim 1, wherein R 1 is (C 4 -C 8 ) alkyl. 2及びR9が水素である、請求項2記載の化合物。 The compound according to claim 2, wherein R 2 and R 9 are hydrogen. XがOである、請求項7記載の化合物。   8. A compound according to claim 7, wherein X is O. YがOR5である、請求項8記載の化合物。 Y is OR 5, wherein compound of claim 8. 5が水素である、請求項9記載の化合物。 R 5 is hydrogen, compound of claim 9. 1が、n−ブチル、n−ペンチル、n−ヘキシル、n−ヘプチル、n−オクチル又はi−ブチルである、請求項10記載の化合物。 11. A compound according to claim 10, wherein R < 1 > is n-butyl, n-pentyl, n-hexyl, n-heptyl, n-octyl or i-butyl. 1がn−ペンチルである、請求項11記載の化合物。 12. A compound according to claim 11 wherein R < 1 > is n-pentyl. 治療上活性な物質として使用するための、請求項1〜12のいずれか1項記載の化合物、又はその塩、溶媒和物若しくは水和物。   13. A compound according to any one of claims 1 to 12, or a salt, solvate or hydrate thereof for use as a therapeutically active substance. 特に気腫、癌又は皮膚障害の処置のための、請求項1〜12のいずれか1項記載の化合物、又はその塩、溶媒和物若しくは水和物を含む、医薬組成物。   A pharmaceutical composition comprising a compound according to any one of claims 1 to 12, or a salt, solvate or hydrate thereof, especially for the treatment of emphysema, cancer or skin disorders. 気腫、癌又は皮膚障害の処置用の薬剤の製造のための、請求項1〜12のいずれか1項記載の化合物、又はその塩、溶媒和物若しくは水和物の使用。   Use of a compound according to any one of claims 1 to 12, or a salt, solvate or hydrate thereof for the manufacture of a medicament for the treatment of emphysema, cancer or skin disorders. 請求項1〜12のいずれか1項記載の化合物、又はその塩、溶媒和物若しくは水和物、及び治療上不活性な担体を含む医薬組成物。   A pharmaceutical composition comprising a compound according to any one of claims 1 to 12, or a salt, solvate or hydrate thereof, and a therapeutically inert carrier. 気腫、癌又は皮膚障害の処置用の、請求項1〜12のいずれか1項記載の化合物、又はその塩、溶媒和物若しくは水和物に基づく薬剤。   A compound based on a compound according to any one of claims 1 to 12, or a salt, solvate or hydrate thereof, for the treatment of emphysema, cancer or skin disorders. 局所又は全身適用のための、請求項17記載の薬剤。   18. A medicament according to claim 17 for local or systemic application. 請求項1記載の化合物又はそのプロ−ドラッグの治療有効量を含む、哺乳動物の気腫、癌又は皮膚障害を処置するための医薬組成物。   A pharmaceutical composition for treating emphysema, cancer or skin disorders in a mammal comprising a therapeutically effective amount of the compound of claim 1 or a pro-drug thereof. 請求項1記載の化合物又はそのプロ−ドラッグを含み、哺乳動物の肺に送達されることを特徴とする、気腫及び関連する障害、癌又は皮膚障害を処置するための配合物。   A composition for treating emphysema and related disorders, cancer or skin disorders, characterized in that it comprises a compound according to claim 1 or a pro-drug thereof and is delivered to the lungs of a mammal.
JP2003528769A 2001-09-18 2002-09-11 Alkylurea retinoid agonist I Expired - Fee Related JP4421293B2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US32296301P 2001-09-18 2001-09-18
PCT/EP2002/010179 WO2003024921A1 (en) 2001-09-18 2002-09-11 Alkyl urea retinoid agonists i

Publications (3)

Publication Number Publication Date
JP2005505571A JP2005505571A (en) 2005-02-24
JP2005505571A5 true JP2005505571A5 (en) 2006-01-05
JP4421293B2 JP4421293B2 (en) 2010-02-24

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JP2003528769A Expired - Fee Related JP4421293B2 (en) 2001-09-18 2002-09-11 Alkylurea retinoid agonist I

Country Status (13)

Country Link
US (1) US6844466B2 (en)
EP (1) EP1430024A1 (en)
JP (1) JP4421293B2 (en)
KR (1) KR100896550B1 (en)
CN (1) CN1283621C (en)
AR (1) AR036533A1 (en)
AU (1) AU2002329276B2 (en)
BR (1) BR0212583A (en)
CA (1) CA2460693C (en)
MX (1) MXPA04002590A (en)
PL (1) PL370361A1 (en)
RU (1) RU2299877C2 (en)
WO (1) WO2003024921A1 (en)

Families Citing this family (11)

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CA2530581A1 (en) * 2003-06-23 2005-01-06 Auspex Pharmaceuticals Novel therapeautic agents for the treatment of cancer, metabolic diseases and skin disorders
WO2005108338A1 (en) * 2004-05-03 2005-11-17 Auspex Pharmaceuticals Novel therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders
JP2008534593A (en) * 2005-03-30 2008-08-28 メルク エンド カムパニー インコーポレーテッド Glucagon receptor antagonist compounds, compositions containing such compounds, and methods of use thereof
TW200821284A (en) * 2006-10-03 2008-05-16 Merck & Co Inc Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use
DK2613776T3 (en) 2010-09-01 2020-10-19 Univ Jefferson COMPOSITION AND METHOD FOR MUSCLE REPAIR AND REGENERATION
WO2014073209A1 (en) 2012-11-08 2014-05-15 国立大学法人山口大学 Therapeutic agent for keratoconjunctive disorders
KR101426197B1 (en) * 2013-02-20 2014-08-01 여윤영 a modeling mold of rice ball
MX362239B (en) 2013-05-22 2019-01-09 Univ Yamaguchi Inhibitor for retinochoroidal disorders.
CN105294567B (en) * 2015-10-29 2018-10-09 湖北新烯王生物科技有限公司 Substituted 3- fluorophenyl methanol classes compound, pharmaceutical composition and purposes
IL295440A (en) 2016-06-08 2022-10-01 Clementia Pharmaceuticals Inc Methods for treating heterotopic ossification
EA039050B1 (en) 2016-11-16 2021-11-26 Клементиа Фармасьютикалс Инк. Methods for treating multiple osteochondroma (mo)

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
LU87821A1 (en) * 1990-10-12 1992-05-25 Cird Galderma BI-AROMATIC COMPOUNDS, AND THEIR USE IN HUMAN AND VETERINARY MEDICINE AND IN COSMETICS
US6093742A (en) 1997-06-27 2000-07-25 Vertex Pharmaceuticals, Inc. Inhibitors of p38
JO2178B1 (en) 1999-10-19 2003-04-23 اف . هوفمان لاروش ايه جي Treatment of emphysema using rar selective retinoid antagonists

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